Microtubule destabilizing agent-2

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Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective antitumor compound targeting microtubule protein. Microtubule destabilizing agent-2 destabilizes microtubule proteins and inhibits microtubule polymers. Microtubule destabilizing agent-2 arrests the G0/G1 phase in human tumor cells. Microtubule destabilizing agent-2 induces Apoptosis by activating the cascade pathway of caspases. Microtubule destabilizing agent-2 has anti-inflammatory activity, as inhibiting TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 reduces tumors growth in xenograft mice.

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Microtubule destabilizing agent-2 Chemical Structure

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Caspase 3

In Vitro

Microtubule destabilizing agent-2 (48 h) has a selective antiproliferative effect on human leukemia cell K-562 (IC₅₀: 3.27 μM), with IC₅₀s of 82.46 μM (MCF-7), 31.27 μM (MDA-MB-231)^[1].
Microtubule destabilizing agent-2 (5 μM, 24 h) induces G0/G1 phase arrest in K562 cells^[1].
Microtubule destabilizing agent-2 (4-64 μM) significantly induces early and late apoptosis in K562 leukemia cells, and activates caspase 3 (activation rate: 2.13 %-26.53 %)^[1].
Microtubule destabilizer-2 (2.5-10 μM, 60 min) destabilizes microtubule proteins^[1].
Microtubule destabilizer-2 (1-10 µg/mL) exhibits moderate anti-inflammatory activity and inhibits LPS (HY-D1056)-induced TNF-α and IL-6 production in primary macrophages^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Microtubule destabilizing agent-2 (20-80 mg/kg, p.o., 28 days) has low to moderate anticancer effects in a K562 xenograft mouse model^[1].
Microtubule destabilizing agent-2 (5-1000 mg/kg, p.o.) induces minor adverse reactions in Swiss albino mice, but is well tolerated^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	K562 xenograft mouse model^[1]
Dosage:	20, 40, 80 mg/kg.
Administration:	Oral gavage (p.o.). 5 days a week for four weeks
Result:	Showed weak anticancer effect at 20 mg/kg (36 % reduction) and 40 mg/kg (31.68 % reduction), but moderate effect at 80 mg/kg (47 %).

Molecular Weight

402.48

Formula

C₂₆H₂₆O₄

SMILES

OC1=C(C2=C(C[C@]([H])(CCC3=C4C=CC(OCC5=CC=CC=C5)=C3)[C@@]24[H])C=C1OC)OC

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Fatima, et al. 5H-benzo[c]fluorene derivative exhibits antiproliferative activity via microtubule destabilization. Bioorganic chemistry, 2024, 153:107891. [Content Brief]